Microwave assisted synthesis and in vitro antimicrobial assessment of quinolone based s-triazines

被引:5
作者
Patel, Divyesh [1 ]
Patel, Rahul [1 ]
Kumari, Premlata [1 ]
Patel, Navin [2 ]
机构
[1] SV Natl Inst Technol, Dept Appl Chem, Surat 395007, India
[2] VN Gujarat Univ, Dept Chem, Surat 395007, India
关键词
antimicrobial activity; microwave irradiation; piperazine; piperidine; quinolone; s-triazine;
D O I
10.1515/HC.2011.006
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of 1,3,5-triazine derivatives that contain aniline, 4-hydroxy-N-methylquinolone and different piperazine and piperidine moieties as substituents on the carbon atoms of the triazine ring has been synthesized by a simple and efficient synthetic protocol. Comparative studies were performed on the compounds, which were synthesized with conventional and microwave heating methods. The microwave method was observed to be more beneficial as it provides an increase in yield and 90%-95% reduction time. The antimicrobial activity of the compounds was tested against seven bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumonia, Salmonella typhi, Proteus vulgaris) and two fungi (Aspergillus niger, Candida albicans). The results indicate that some of the novel s-triazines have noteworthy activity in MIC and agar diffusion tests.
引用
收藏
页码:33 / 41
页数:9
相关论文
共 21 条
  • [1] Anastasia D., 2007, J MED CHEM, V50, P2450
  • [2] Design and synthesis of a series of melamine-based nitroheterocycles with activity against trypanosomatid parasites
    Baliani, A
    Bueno, GJ
    Stewart, ML
    Yardley, V
    Brun, R
    Barrett, MP
    Gilbert, IH
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (17) : 5570 - 5579
  • [3] Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization. A promising alternative to random screening
    Boehm, HJ
    Boehringer, M
    Bur, D
    Gmuender, H
    Huber, W
    Klaus, W
    Kostrewa, D
    Kuehne, H
    Luebbers, T
    Meunier-Keller, N
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) : 2664 - 2674
  • [4] Mechanism of action of eukaryotic topoisomerase II and drugs targeted to the enzyme
    Burden, DA
    Osheroff, N
    [J]. BIOCHIMICA ET BIOPHYSICA ACTA-GENE STRUCTURE AND EXPRESSION, 1998, 1400 (1-3): : 139 - 154
  • [5] Efficient synthesis of 2-substituted 2,3-dihydro-4-quinolones as potential intermediates for 2-substituted 1,2,3,4-tetrahydro-4-quinolone antitumor agents
    Choi, Sun
    Jung, Keumnyeo
    Ryu, Jaesang
    [J]. ARCHIVES OF PHARMACAL RESEARCH, 2006, 29 (05) : 369 - 374
  • [6] CLEMENT JJ, 1995, CANCER RES, V55, P830
  • [7] Cruickshank R, 1975, MED MICROBIOLGY
  • [8] Drlica K, 1999, CURR OPIN ANTIINFECT, V1, P435
  • [9] QSAR study and VolSurf characterization of anti-HIV quinolone library
    Filipponi, E
    Cruciani, G
    Tabarrini, O
    Cecchetti, V
    Fravolini, A
    [J]. JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 2001, 15 (03) : 203 - 217
  • [10] Kappe CO, 2005, METH PRIN MED CHEM, V52, P1, DOI 10.1002/3527606556